摘要
舒他西林为舒巴坦和氨苄西林的双酯甲苯磺酸盐,口服吸收后在体内以氨苄西林和舒巴坦单体产生抗菌作用。舒巴坦是β-内酰胺酶的高效不可逆抑制剂,与氨苄西林合用,增加了氨苄西林对一些产β-内酰胺酶耐药菌的抗菌活性。舒他西林对常见的大多数细菌均有较强的抗菌活性,其MIC_(50)和MIC_(90)为氨苄西林的1/2～1/64,其MBC为MIC的1～4倍,明显优于氨苄西林。舒巴坦和氨苄西林的药代动力学特性基本相同,在血液、体液和组织中可达高浓度。口服舒他西林的抗菌活性和临床有效性与肠道外给药的舒巴坦/氨苄西林复方的效果类似。舒他西林对呼吸道、耳鼻喉、尿道、皮肤软组织、妇产科等各种感染及淋病均有较好疗效。临床药物不良反应发生率低且均为轻度和暂时性的,典型的药物不良反应为腹泻和稀便。
Sultamicillin is the tosylate salt of the double ester of sulbactum plus ampicillin. Tt is hydrolyzed by enzymes in the intestinal wall after orally administered, releasing sulbactum and ampicillin in equimolar proportions. Sulbactum is an ef fective irreversible semisynthetic inhibitor unique for β- lactamase, when in combination with ampicillin, which extends the antibacterial activity of the latter including some β - lactamawe - producing strains of bacteria that would otherwise be resistant. The antibacterial activity of sultamicillin against most of bacteria was 2 - 64 times stronger than that of ampicillin. A close relationship exists between the pharmacokinetic handling of both sulbactum and ampicillin. Both time to peak plasma concentration (approximate 1 hour) and profile of elimination are similar for two drugs. Sultamicillin had much higher bactericidal activity than that of ampicillin arid sulbactum(1 : 1). Sultarnicillin has been shown to be clinically ef fective in non - comparative trials in patients with infection of the respiratory tract, nose and throat, urinary tract, shin and soft tissues, as in obstetric and gynecological infections and in the treatment of gonorrhea. The overall incidence of adverse reaction reported was 7.2% (3 005 cases), the typical symptoms with an incidence of greater than 1% was diarrhoea (3. 7% ) and soft stools (1. 1% ).
出处
《中国医药导刊》
2000年第4期34-35,37,共3页
Chinese Journal of Medicinal Guide
